valemetostat 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
histone N-methyltransferase inhibitors 5724 1809336-39-7

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • valemetostat
  • valemetostat tosilate
  • ezharmia
  • DS-3201
Valemetostat is a drug that blocks two enzymes called EZH1 and EZH2. These enzymes are involved in the growth of some blood cancers and solid tumors, such as non-Hodgkin lymphomas (NHL). Valemetostat is used to treat a type of NHL called adult T-cell leukaemia/lymphoma (ATL) that has come back or does not respond to other treatments.
  • Molecular weight: 488.03
  • Formula: C26H34ClN3O4
  • CLOGP:
  • LIPINSKI: 0
  • HAC: 7
  • HDO: 2
  • TPSA: 79.90
  • ALOGS:
  • ROTB: 5

Drug dosage:

None

ADMET properties:

None

Approvals:

DateAgencyCompanyOrphan
Sept. 26, 2022 PMDA DAIICHI SANKYO COMPANY, LIMITED

FDA Adverse Event Reporting System (Female)

None

FDA Adverse Event Reporting System (Male)

None

FDA Adverse Event Reporting System (Geriatric)

None

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

None

Drug Use | Suggest Off label Use Form| |View source of the data|

DiseaseRelationSNOMED_IDDOID
Relapsed or refractory T-cell leukemia-lymphoma indication 110007008 DOID:5603




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

None

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Histone-lysine N-methyltransferase EZH2 Enzyme INHIBITOR IC50 8.22 SCIENTIFIC LITERATURE
Histone-lysine N-methyltransferase EZH1 Enzyme INHIBITOR IC50 8 SCIENTIFIC LITERATURE

External reference:

IDSource
CHEMBL4597193 ChEMBL_ID
12282 IUPHAR_LIGAND_ID
C5239419 UMLSCUI
CHEMBL4594405 ChEMBL_ID
10747 INN_ID
126481870 PUBCHEM_CID
D11551 KEGG_DRUG
60RD0234VE UNII

Pharmaceutical products:

None